| Stem definition | Drug id | CAS RN |
|---|---|---|
| local anaesthetics | 1097 | 36637-18-0 |
None
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 24.13 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 0 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 30, 1976 | FDA |
None
None
None
None
| Source | Code | Description |
|---|---|---|
| ATC | N01BB07 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Amides |
| ATC | N01BB57 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, LOCAL Amides |
| CHEBI has role | CHEBI:36333 | local anesthetics |
| MeSH PA | D000777 | Anesthetics |
| MeSH PA | D000779 | Anesthetics, Local |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018689 | Sensory System Agents |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Sinus tachycardia | contraindication | 11092001 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Parkinsonism | contraindication | 32798002 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Cerebral arteriosclerosis | contraindication | 65312002 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Cardiogenic shock | contraindication | 89138009 | |
| Bleeding | contraindication | 131148009 | |
| Angina pectoris | contraindication | 194828000 | |
| Primary dilated cardiomyopathy | contraindication | 195021004 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Disorder of coronary artery | contraindication | 414024009 |
None
None
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.24 | acidic |
| pKa2 | 7.84 | Basic |
None
None
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sodium channel protein type 5 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL | |||||
| Sodium channel protein type 2 subunit alpha | Ion channel | BLOCKER | UNKNOWN | CHEMBL | |||||
| Sodium channel protein type 4 subunit alpha | Ion channel | BLOCKER | WOMBAT-PK | CHEMBL | |||||
| Potassium channel subfamily K member 3 | Ion channel | IC50 | 4.41 | CHEMBL | |||||
| Sodium channel protein type 2 subunit alpha | Ion channel | BLOCKER | IC50 | 6 | IUPHAR |
| ID | Source |
|---|---|
| 4019752 | VUID |
| N0000147843 | NUI |
| D04095 | KEGG_DRUG |
| 36637-19-1 | SECONDARY_CAS_RN |
| 4018912 | VANDF |
| 4019752 | VANDF |
| C0015120 | UMLSCUI |
| CHEBI:4904 | CHEBI |
| CHEMBL492 | ChEMBL_ID |
| DB08987 | DRUGBANK_ID |
| D005041 | MESH_DESCRIPTOR_UI |
| 37497 | PUBCHEM_CID |
| 2621 | IUPHAR_LIGAND_ID |
| 3419 | INN_ID |
| I6CQM0F31V | UNII |
| 227221 | RXNORM |
| 4705 | MMSL |
| d01400 | MMSL |
| 001339 | NDDF |
| 005119 | NDDF |
| 370282009 | SNOMEDCT_US |
| 4043008 | SNOMEDCT_US |
| 88485001 | SNOMEDCT_US |
| CHEMBL1200597 | ChEMBL_ID |
None